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11. 发明申请

US20090006059A1 Systems and methods for mapping binding site volumes in macromolecules 审中-公开
标题翻译：在大分子中映射结合位点体积的系统和方法
公开(公告)号：US20090006059A1
公开(公告)日：2009-01-01
申请号：US11823697
申请日：2007-06-27
申请人： Nidhi Arora , Chris Williams
发明人： Nidhi Arora , Chris Williams
IPC分类号： G06G7/48
CPC分类号： G16B15/00
摘要： Systems, methods, and apparatus for evaluating a binding site of a macromolecule are disclosed in which the binding site is identified and a binding site volume map of the binding site is constructed. The binding site volume map has a surface with a plurality of regions. Each respective region in the plurality of regions of the surface is classified based upon a first characteristic that is complementary to a second characteristic of a portion of the macromolecule that is nearest to the respective region, thereby creating an interaction map. Systems, methods, and apparatus for comparing macromolecules are also disclosed in which a binding site volume map is constructed for each of the macromolecules. Then, a composite binding site volume map that comprises a volumetric combination of each of the binding site volume maps is constructed. An interaction map can be constructed from the composite binding site volume map.
摘要翻译：公开了用于评估大分子的结合位点的系统，方法和装置，其中鉴定了结合位点并构建了结合位点的结合位点体积图。结合位点体积图具有具有多个区域的表面。基于与最接近各个区域的大分子的一部分的第二特征互补的第一特征，对表面的多个区域中的每个区域进行分类，由此形成交互图。还公开了用于比较大分子的系统，方法和装置，其中为每个大分子构建结合位点体积图。然后，构建包含每个结合位点体积图的体积组合的复合结合位点体积图。可以从复合绑定站点卷映射构建交互图。

12. 发明申请

US20140364595A1 CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS 有权
标题翻译：基于连接的抗真菌和抗菌素PRODRUGS
公开(公告)号：US20140364595A1
公开(公告)日：2014-12-11
申请号：US14128281
申请日：2012-06-22
申请人： Abhijit S. Bapat , Gauthami Mahesh , Rajesh S. Gokhale , Sayali S. Shah , Shiladitya Sengupta , Sudhanand Prasad , Sumana Ghosh , Suresh R. Chawrai , Nidhi Arora , D. Sreedhar Reddy , Malika Mishra , Kirti Bajaj
发明人： Abhijit S. Bapat , Gauthami Mahesh , Rajesh S. Gokhale , Sayali S. Shah , Shiladitya Sengupta , Sudhanand Prasad , Sumana Ghosh , Suresh R. Chawrai , Nidhi Arora , D. Sreedhar Reddy , Malika Mishra , Kirti Bajaj
IPC分类号： A61K31/7056 , A61K47/48 , A61K31/085 , A61K31/496
CPC分类号： A61K31/7056 , A01N37/46 , A61K8/0241 , A61K8/347 , A61K8/361 , A61K8/362 , A61K8/368 , A61K8/37 , A61K8/375 , A61K8/39 , A61K8/49 , A61K8/4933 , A61K8/602 , A61K8/8129 , A61K31/085 , A61K31/496 , A61K47/54 , A61K47/542 , A61K47/552 , A61K47/60 , A61K2800/412 , A61K2800/413 , A61K2800/57 , A61Q5/006 , A61Q17/005
摘要： The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
摘要翻译：本发明提供了通过将至少一种抗真菌剂或抗菌剂与至少一种接头和/或载体偶联而形成的基于缀合物的抗真菌或抗菌前药。前药具有下式：（i）（AFA）m-X-（L）n; （ii）[（AFA）m'-X] p-L; （iii）AFA- [X-（L）n'] q; 或（iv）（AFA）m“-X，其中：AFA是抗真菌剂或抗菌剂; L是载体; X是一个连接子; m范围从1到10; n范围从2到10; m'为1〜10; p为1〜10; n'为1〜10; q为1〜10，条件是q'和n不同时为1; 并且m“为1至10.本发明还提供了包含基于缀合物的前药的纳米颗粒。此外，本发明还提供纳米颗粒形式的非共轭抗真菌剂和抗菌剂。

13. 发明申请

US20100056535A1 Inhibitors of HIV-1 reverse transcriptase 审中-公开
标题翻译： HIV-1逆转录酶抑制剂
公开(公告)号：US20100056535A1
公开(公告)日：2010-03-04
申请号：US12584436
申请日：2009-09-04
申请人： Nidhi Arora , Roland Joseph Billedeau , Joshua Kennedy-Smith , Weiling Liang , Ralf Roetz , Zachary Kevin Sweeney
发明人： Nidhi Arora , Roland Joseph Billedeau , Joshua Kennedy-Smith , Weiling Liang , Ralf Roetz , Zachary Kevin Sweeney
IPC分类号： A61K31/501 , C07D217/06 , C07D403/06 , A61K31/4709 , A61K31/4439 , A61P31/18
CPC分类号： C07D401/06 , C07D213/69 , C07D213/74 , C07D413/06
摘要： The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to Formulae I and II wherein Q, R1, R2, and R3 are defined as described herein.
摘要翻译：本发明提供了用于治疗或预防HIV感染或治疗AIDS或ARC的化合物，其包括给予根据式I和II的化合物，其中Q，R 1，R 2和R 3如本文所述定义。

14. 发明授权

US09907812B2 Conjugate-based antifungal and antibacterial prodrugs 有权
公开(公告)号：US09907812B2
公开(公告)日：2018-03-06
申请号：US14128281
申请日：2012-06-22
申请人： Abhijit S. Bapat , Gauthami Mahesh , Rajesh S. Gokhale , Sayali S. Shah , Shiladitya Sengupta , Sudhanand Prasad , Sumana Ghosh , Suresh R. Chawrai , Nidhi Arora , D. Sreedhar Reddy , Mallika Mishra , Kirti Bajaj
发明人： Abhijit S. Bapat , Gauthami Mahesh , Rajesh S. Gokhale , Sayali S. Shah , Shiladitya Sengupta , Sudhanand Prasad , Sumana Ghosh , Suresh R. Chawrai , Nidhi Arora , D. Sreedhar Reddy , Mallika Mishra , Kirti Bajaj
IPC分类号： A61K31/7056 , A61K47/48 , A61K31/085 , A61K31/496 , A61K8/37 , A61Q17/00 , A61K8/34 , A61K8/36 , A61K8/362 , A61K8/368 , A61K8/39 , A61K8/49 , A61Q5/00 , A61K8/60 , A61K8/81 , A61K8/02 , A01N37/46 , A61K47/60 , A61K47/54 , A61K47/55
CPC分类号： A61K31/7056 , A01N37/46 , A61K8/0241 , A61K8/347 , A61K8/361 , A61K8/362 , A61K8/368 , A61K8/37 , A61K8/375 , A61K8/39 , A61K8/49 , A61K8/4933 , A61K8/602 , A61K8/8129 , A61K31/085 , A61K31/496 , A61K47/54 , A61K47/542 , A61K47/552 , A61K47/60 , A61K2800/412 , A61K2800/413 , A61K2800/57 , A61Q5/006 , A61Q17/005
摘要： The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.

15. 发明申请

US20120015962A1 PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS 审中-公开
标题翻译：吡咯并[1,5a]吡嗪衍生物作为IRAK4调节剂
公开(公告)号：US20120015962A1
公开(公告)日：2012-01-19
申请号：US13180589
申请日：2011-07-12
申请人： Nidhi Arora , Shaoqing Chen , Johannes Cornelius Hermann , Adreas Kuglstatter , Sharada Shenvi Labadie , Clara Jeou Jen Lin , Matthew C. Lucas , Amy Geraldine Moore , Eva Papp , Francisco Xavier Talamas , Jutta Wanner , Yansheng Zhai
发明人： Nidhi Arora , Shaoqing Chen , Johannes Cornelius Hermann , Adreas Kuglstatter , Sharada Shenvi Labadie , Clara Jeou Jen Lin , Matthew C. Lucas , Amy Geraldine Moore , Eva Papp , Francisco Xavier Talamas , Jutta Wanner , Yansheng Zhai
IPC分类号： A61K31/519 , C07D495/04 , A61P19/02 , A61P11/00 , A61P11/06 , A61P11/08 , C07D487/04 , A61K31/4365
CPC分类号： C07D495/04 , C07D487/04
摘要： Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
摘要翻译：式I或II的化合物：其中X，m，Ar，R 1和R 2如本文所定义。本发明化合物可用于治疗IRAK介导的病症。

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